Inclusion of an antiplatelet agent inside into β-cyclodextrin for biochemical applications with diverse authentications

• Published in: Food chemistry advances Vol. 1; p. 100015
• Main Authors: Bomzan, Pranish, Roy, Niloy, Rai, Vijeta, Roy, Debadrita, Ghosh, Shilpi, Kumar, Anoop, Roy, Kanak, Chakrabarty, Rinku, Das, Jyotsna, Dakua, Vikas Kumar, Basnet, Kumar, Roy, Mahendra Nath
• Format: Journal Article
• Language: English
• Published: Elsevier Ltd 01.10.2022; Elsevier
• Subjects: Antibacterial activity; Cytotoxicity; Molecular docking; Thermogravimetric analysis; Ticlopidine hydrochloride; β-cyclodextrin; TCP; β-CD; FDA; Thermogravimetric analysis; ACHN; ROS; Antibacterial activity; Cytotoxicity; β-cyclodextrin; Molecular docking; Ticlopidine hydrochloride
• ISSN: 2772-753X; 2772-753X
• DOI: 10.1016/j.focha.2022.100015

•The TCP-β-CD complex was found to have 1:1 stoichiometry.•The complexation process was found to be thermodynamically favorable.•Inclusion into β-CD enhances the thermal stability of TCP.•Molecular level interactions in TCP-β-CD complex were studied by molecular docking method.•TCP-β-CD complex showed better antibacterial efficacy and cytotoxic effect than pure TCP. We aim to develop the complex of ticlopidine hydrochloride (TCP) with β-cyclodextrin (β-CD) and to investigate its antibacterial and cytotoxic activities. The complex was characterized by various physicochemical as well as spectroscopic techniques suggesting the successful inclusion of TCP molecule into the β-CD cavity. TG analysis showed that the thermal stability of TCP was found to improve after complexation. Molecular docking study speculated the most preferred orientation of TCP molecule within the binding pocket of β-CD cavity. In vitro antibacterial activity test demonstrated that the TCP-β-CD complex displayed better activity than pure TCP. TCP-β-CD complex (IC50 = 24 μM) also exhibited significant in vitro cytotoxic activity than pure TCP (IC50 = 44 μM) towards human kidney cancer cell line (ACHN). Furthermore, the complex induces the ROS generation in ACHN cells more pronouncedly than TCP alone, suggesting the increased apoptotic activity of TCP after complexation. These results reveals that inclusion of TCP using β-CD could lead to stabilization of TCP and efficient display of its antibacterial and cytotoxic activities.